Name | Toceranib Phosphate |
CAS number | 874819-74-6 |
Description | Toceranib Phosphate is a small molecule, orally bioavailable receptor tyrosine kinase inhibitor, developed specifically for veterinary oncology, with the CAS Registry Number 874819-74-6. |
Structural formula |  |
Molecular Formula | C22H28FN4O6P |
Molecular Weight | 494.46 g/mol |
Appearance | White powder |
Quality Standard | 99% |
Storage Condition | Cool dry place( away from the light) |
Shelf Life | >2 years if stored properly |
Sample package | Aluminium foil bag |
Commercial package | Aluminium Tin, Fiber drum |
Origin | China |
Toceranib Phosphate More Info
Toceranib Phosphate is a small molecule, orally bioavailable receptor tyrosine kinase inhibitor, developed specifically for veterinary oncology, with the CAS Registry Number 874819-74-6. Its molecular structure is based on an indolinone core, designed to competitively inhibit the ATP-binding site of specific tyrosine kinase receptors. The phosphate salt formulation enhances its solubility and stability for pharmaceutical manufacturing. It represents a pioneering example of a targeted cancer therapy developed and approved explicitly for companion animals.
The primary mechanism of action involves the selective inhibition of a range of split-kinase domain receptor tyrosine kinases. Its key targets include platelet-derived growth factor receptor, vascular endothelial growth factor receptor, and stem cell factor receptor. By blocking the signaling pathways of these receptors, which are often dysregulated in mast cell tumors and other cancers, toceranib inhibits tumor cell proliferation, disrupts tumor-associated angiogenesis, and promotes apoptosis. This multi-targeted approach directly addresses the molecular drivers of certain canine cancers.
The main clinical application of toceranib phosphate is the treatment of non-resectable, recurrent, or metastatic canine mast cell tumors. It is specifically indicated for dogs with Patnaik grade 2 or 3 MCTs that have demonstrated c-Kit mutations, a key predictor of response. It is also used in the management of other malignancies, such as certain types of sarcoma and carcinoma in dogs, where its anti-angiogenic and antiproliferative effects provide clinical benefit. Its development marked a significant advancement in veterinary oncology, offering a targeted oral therapeutic option.
This medication is administered orally in tablet form, typically on an intermittent dosing schedule such as every other day or a Monday-Wednesday-Friday regimen. This schedule is designed to manage potential side effects while maintaining antitumor efficacy. It is metabolized in the liver and has a half-life suitable for intermittent dosing. Dosing is based on the dog's body surface area, and treatment requires regular veterinary monitoring, including physical examinations and blood work, to assess response and manage toxicity.
The safety profile of toceranib includes manageable but notable side effects. The most common adverse effects are gastrointestinal, including diarrhea, vomiting, anorexia, and lethargy, which are often dose-dependent and may require supportive care or dose adjustments. More serious but less frequent risks include neutrophilia, proteinuria, and delayed wound healing. Its targeted nature generally results in fewer severe systemic toxicities compared to traditional chemotherapy. Its use is contraindicated in breeding animals and requires careful risk-benefit assessment by a veterinary oncologist.
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